An enzymatic [4+2] cyclization cascade creates the pentacyclic core of pyrroindomycins

Nat Chem Biol. 2015 Apr;11(4):259-65. doi: 10.1038/nchembio.1769. Epub 2015 Mar 2.

Abstract

The [4+2] cycloaddition remains one of the most intriguing transformations in synthetic and natural products chemistry. In nature, however, there are remarkably few enzymes known to have this activity. We herein report an unprecedented enzymatic [4+2] cyclization cascade that has a central role in the biosynthesis of pyrroindomycins, which are pentacyclic spirotetramate natural products. Beginning with a linear intermediate that contains two pairs of 1,3-diene and alkene groups, the dedicated cyclases PyrE3 and PyrI4 act in tandem to catalyze the formation of two cyclohexene rings in the dialkyldecalin system and the tetramate spiro-conjugate of the molecules. The two cyclizations are completely enzyme dependent and proceed in a regio- and stereoselective manner to establish the enantiomerically pure pentacyclic core. Analysis of a related spirotetronate pathway confirms that homologs are functionally exchangeable, establishing the generality of these findings and explaining how nature creates diverse active molecules with similar rigid scaffolds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry
  • Biological Products / chemistry
  • Catalysis
  • Chemistry / methods*
  • Cyclization
  • Cyclohexenes / chemistry
  • DNA, Bacterial / chemistry
  • Intramolecular Lyases / chemical synthesis
  • Intramolecular Lyases / chemistry*
  • Macrolides / chemical synthesis*
  • Macrolides / chemistry
  • Models, Chemical
  • Molecular Structure
  • Mutation
  • Plasmids / metabolism
  • Pyrrolidinones / chemical synthesis
  • Pyrrolidinones / chemistry*
  • Recombinant Proteins / chemistry
  • Stereoisomerism
  • Streptomyces / metabolism

Substances

  • Alkenes
  • Biological Products
  • Cyclohexenes
  • DNA, Bacterial
  • Macrolides
  • Pyrrolidinones
  • Recombinant Proteins
  • Intramolecular Lyases

Associated data

  • PubChem-Substance/226392643
  • PubChem-Substance/226392644
  • PubChem-Substance/226392645
  • PubChem-Substance/226392646